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Polymorphic substances of triaryl dimethyl piperazine hydrobromide, and preparation method and application thereof

A technology of dimethylpiperazine and ketone hydrobromide, applied in the field of medicine, can solve problems such as inability to concentrate, sexual dysfunction, long onset time, and confusion of thinking, and achieve the prevention and treatment of depression and other potential diseases, good stability and high bioavailability

Inactive Publication Date: 2017-04-26
YUNNAN INST OF MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drugs, while effective, often have problematic side effects, such as lethargy, confusion, inability to concentrate, and sexual dysfunction
Also, these drugs suffer from long onset times, requiring about 6 to 8 weeks to show any desired therapeutic effect

Method used

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  • Polymorphic substances of triaryl dimethyl piperazine hydrobromide, and preparation method and application thereof
  • Polymorphic substances of triaryl dimethyl piperazine hydrobromide, and preparation method and application thereof
  • Polymorphic substances of triaryl dimethyl piperazine hydrobromide, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl) Preparation of polymorph A of methyl) phenyl) (4-methylpiperidin-1-yl) ketone hydrobromide

[0047] Take 2g of (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl base) phenyl) (4-methylpiperidin-1-yl) ketone into a glass bottle, add 15 mL of acetone into the glass bottle, stir evenly, then add 1 mL of hydrobromic acid with a volume percentage of 40%, and stir at room temperature , reacted for 16 hours, filtered and dried to obtain (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl )(3-hydroxyphenyl)methyl)phenyl)(4-methylpiperidin-1-yl)methanone hydrobromide polymorph A.

[0048] (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxy The XRPD pattern of polymorph A of phenyl) methyl) phenyl) (4-methylpiperidin-1-yl) ketone hydrobromide figure 1 The peak information of its spectrum is shown in Table 1. TGA ...

Embodiment 2

[0051] Example 2 (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl) Preparation of polymorph B of methyl)phenyl)(4-methylpiperidin-1-yl)methanone hydrobromide

[0052] (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3- The polymorph A of hydroxyphenyl)methyl)phenyl)(4-methylpiperidin-1-yl)methanone hydrobromide was used as the starting sample, heated to 100°C, and collected after constant temperature for 5 minutes The solid is polymorph B.

[0053] (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazin-1-yl)(3-hydroxy The XRPD pattern of polymorph B of phenyl)methyl)phenyl)(4-methylpiperidin-1-yl)methanone hydrobromide is shown in image 3 The peak information of its spectrum is shown in Table 2. TGA and DSC diagrams of polymorph B Figure 4 shown by Figure 4 It can be seen that the melting point of polymorph B is 174.2°C (the melting range is 165.8°C-174.2°C as judged from DSC).

[0054] Table 2 XRPD peak information...

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Abstract

The invention discloses two polymorphic substances A and B of (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazine-1-yl)(3-hydroxylbenzyl)methyl)phenyl)(4-methylpiperidine-1-yl)ketone hydrobromide; and a preparation method and an application thereof in the preparation of drugs for preventing or treating mood disorder or diseases related with a delta opioid receptor.

Description

technical field [0001] The present invention relates to, but not limited to, the technical field of medicine, in particular, relates to but not limited to a triaryl dimethyl piperazine hydrobromide multi-crystal form and its preparation method and application. Background technique [0002] Depression is a common mental illness, mainly manifested as low mood, loss of interest, pessimism, slow thinking, lack of initiative, self-blame, poor diet and sleep, worry that you have various diseases, and feeling that you are suffering from various diseases in your body. Discomfort, and in severe cases, suicidal thoughts and behaviors may appear. In the fourth edition of the "Diagnostic and Statistical Manual of Mental Disorders" published by the American Psychiatric Association, depression is classified under mood disorders and is divided into three types: major depressive disorder, dysthymic disorder and other Unspecified depression. [0003] Factors causing depression include: gen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/10A61K31/496A61P25/24A61P25/04A61P29/00A61P25/22A61P1/04A61P25/00
CPCC07D401/10C07B2200/13
Inventor 王京昆宋鹤孙敏王泽人杨志苏敏刘红斌师冰毛勇刘慧浪李泽千崔涛赵春梅苏梅袁芳张天财刘勇张宽仁魏云林沈悦海
Owner YUNNAN INST OF MATERIA MEDICA
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